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Spray freeze drying with polyvinylpyrrolidone and sodium caprate for improved dissolution and oral bioavailability of oleanolic acid, a BCS Class IV compound
Tong H.H.Y.1; Du Z.2; Wang G.N.3; Chan H.M.1; Chang Q.3; Lai L.C.M.2; Chow A.H.L.4; Zheng Y.2
2011-02-14
Source PublicationInternational Journal of Pharmaceutics
ISSN0378-5173
Volume404Issue:1-2Pages:148-158
Abstract

Spray-freeze-drying (SFD) of oleanolic acid (OA), a BCS Class IV compound, with polyvinylpyrrolidone-40 (PVP-40) as stabilizer and sodium caprate (SC) as wetting agent and penetration enhancer produced kinetically stable, amorphous solid dispersion systems with superior in vitro dissolution performance, and better and more uniform absorption in comparison with commercial OA tablet. Relative to the SC-free formulation, the presence of SC in the formulation resulted in a significant increase in the in vivo absorption rate of OA while exerting no apparent impact on the extent of OA absorption. The SFD-processed OA formulations and commercial OA tablet generally exhibited large inter-animal variability in oral bioavailability, consistent with the absorption characteristics of BCS Class IV compounds. Inclusion of SC coupled with the replacement of OA with its sodium salt (OA-Na) in the formulation was shown to substantially decrease the observed absorption variability. Above results suggested that increases in both dissolution rate and intestinal permeability of BCS Class IV compounds, as exemplified by the SFD-processed dispersion system containing both OA-Na and SC, are critical to reducing the large inter-individual absorption variability commonly observed with this class of drugs. 

KeywordDissolution Oleanolic Acid Oral Bioavailability Sodium Caprate Sodium Oleanolate Spray Freeze Drying
DOIhttps://doi.org/10.1016/j.ijpharm.2010.11.027
URLView the original
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000289220400019
The Source to ArticleScopus
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Cited Times [WOS]:45   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorChow A.H.L.; Zheng Y.
Affiliation1.School of Health Sciences, Macao Polytechnic Institute, Macao
2.Institute of Chinese Medical Sciences, University of Macau, Macao
3.Institute of Medicinal Plant Development, Chinese Academy of Medical Science & Peking Union Medical College, Beijing 100193, China
4.School of Pharmacy, The Chinese University of Hong Kong, Hong Kong, China
Corresponding Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Tong H.H.Y.,Du Z.,Wang G.N.,et al. Spray freeze drying with polyvinylpyrrolidone and sodium caprate for improved dissolution and oral bioavailability of oleanolic acid, a BCS Class IV compound[J]. International Journal of Pharmaceutics,2011,404(1-2):148-158.
APA Tong H.H.Y..,Du Z..,Wang G.N..,Chan H.M..,Chang Q..,...&Zheng Y..(2011).Spray freeze drying with polyvinylpyrrolidone and sodium caprate for improved dissolution and oral bioavailability of oleanolic acid, a BCS Class IV compound.International Journal of Pharmaceutics,404(1-2),148-158.
MLA Tong H.H.Y.,et al."Spray freeze drying with polyvinylpyrrolidone and sodium caprate for improved dissolution and oral bioavailability of oleanolic acid, a BCS Class IV compound".International Journal of Pharmaceutics 404.1-2(2011):148-158.
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